TW200900080A - Mineralcorticoid receptor antagonists for the treatment of endometriosis - Google Patents
Mineralcorticoid receptor antagonists for the treatment of endometriosis Download PDFInfo
- Publication number
- TW200900080A TW200900080A TW097107235A TW97107235A TW200900080A TW 200900080 A TW200900080 A TW 200900080A TW 097107235 A TW097107235 A TW 097107235A TW 97107235 A TW97107235 A TW 97107235A TW 200900080 A TW200900080 A TW 200900080A
- Authority
- TW
- Taiwan
- Prior art keywords
- receptor antagonist
- mineral corticosteroid
- mineral
- estrogen
- endometriosis
- Prior art date
Links
- 201000009273 Endometriosis Diseases 0.000 title claims abstract description 46
- 238000011282 treatment Methods 0.000 title claims abstract description 42
- 239000002395 mineralocorticoid Substances 0.000 title claims description 78
- 229940044551 receptor antagonist Drugs 0.000 title claims description 54
- 239000002464 receptor antagonist Substances 0.000 title claims description 54
- 239000003814 drug Substances 0.000 claims abstract description 12
- 102000007451 Steroid Receptors Human genes 0.000 claims description 76
- 108091008723 corticosteroid receptors Proteins 0.000 claims description 76
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 27
- 239000000262 estrogen Substances 0.000 claims description 14
- 229940011871 estrogen Drugs 0.000 claims description 14
- 229960003387 progesterone Drugs 0.000 claims description 12
- 239000000186 progesterone Substances 0.000 claims description 12
- 102000005962 receptors Human genes 0.000 claims description 12
- 108020003175 receptors Proteins 0.000 claims description 12
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical group C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 claims description 12
- 229960002256 spironolactone Drugs 0.000 claims description 12
- 239000003446 ligand Substances 0.000 claims description 11
- 239000000583 progesterone congener Substances 0.000 claims description 11
- 229940123788 Progesterone receptor antagonist Drugs 0.000 claims description 9
- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 claims description 8
- 108010038795 estrogen receptors Proteins 0.000 claims description 8
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 claims description 7
- 229960004845 drospirenone Drugs 0.000 claims description 7
- 239000003862 glucocorticoid Substances 0.000 claims description 7
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims description 7
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims description 7
- 230000009471 action Effects 0.000 claims description 6
- 239000003098 androgen Substances 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 6
- 229960001208 eplerenone Drugs 0.000 claims description 6
- 239000000849 selective androgen receptor modulator Substances 0.000 claims description 6
- 210000003802 sputum Anatomy 0.000 claims description 6
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims description 5
- 206010036790 Productive cough Diseases 0.000 claims description 5
- JUKPWJGBANNWMW-VWBFHTRKSA-N eplerenone Chemical group C([C@@H]1[C@]2(C)C[C@H]3O[C@]33[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)C(=O)OC)C[C@@]21CCC(=O)O1 JUKPWJGBANNWMW-VWBFHTRKSA-N 0.000 claims description 5
- 208000024794 sputum Diseases 0.000 claims description 5
- 229940030486 androgens Drugs 0.000 claims description 4
- 230000002280 anti-androgenic effect Effects 0.000 claims description 4
- 239000000051 antiandrogen Substances 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- 229940077150 progesterone and estrogen Drugs 0.000 claims description 4
- 229940037128 systemic glucocorticoids Drugs 0.000 claims description 4
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 2
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical group OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 2
- 229960002568 ethinylestradiol Drugs 0.000 claims description 2
- 102000015694 estrogen receptors Human genes 0.000 claims 3
- 239000002379 progesterone receptor modulator Substances 0.000 claims 2
- 241000233866 Fungi Species 0.000 claims 1
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 abstract description 5
- 210000000988 bone and bone Anatomy 0.000 abstract description 4
- 239000000203 mixture Substances 0.000 abstract description 3
- 238000002560 therapeutic procedure Methods 0.000 abstract description 2
- 229940083712 aldosterone antagonist Drugs 0.000 abstract 2
- 230000002349 favourable effect Effects 0.000 abstract 1
- 239000002394 mineralocorticoid antagonist Substances 0.000 abstract 1
- 230000003902 lesion Effects 0.000 description 33
- 230000000694 effects Effects 0.000 description 24
- 210000001519 tissue Anatomy 0.000 description 17
- 210000004696 endometrium Anatomy 0.000 description 15
- 241000237858 Gastropoda Species 0.000 description 10
- 230000002357 endometrial effect Effects 0.000 description 10
- 229910052500 inorganic mineral Inorganic materials 0.000 description 10
- 239000011707 mineral Substances 0.000 description 10
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 description 9
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 description 9
- 241001465754 Metazoa Species 0.000 description 9
- 229960002478 aldosterone Drugs 0.000 description 9
- 102100038595 Estrogen receptor Human genes 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- 210000004291 uterus Anatomy 0.000 description 7
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 6
- 229930182833 estradiol Natural products 0.000 description 6
- 229960005309 estradiol Drugs 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 102000003998 progesterone receptors Human genes 0.000 description 6
- 108090000468 progesterone receptors Proteins 0.000 description 6
- 241000282560 Macaca mulatta Species 0.000 description 5
- 230000027758 ovulation cycle Effects 0.000 description 5
- 230000008092 positive effect Effects 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 229940083324 Selective androgen receptor modulator Drugs 0.000 description 4
- 239000000556 agonist Substances 0.000 description 4
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 230000006870 function Effects 0.000 description 4
- 230000035935 pregnancy Effects 0.000 description 4
- 230000035755 proliferation Effects 0.000 description 4
- 230000009467 reduction Effects 0.000 description 4
- 238000003757 reverse transcription PCR Methods 0.000 description 4
- 238000002054 transplantation Methods 0.000 description 4
- WOVKYSAHUYNSMH-RRKCRQDMSA-N 5-bromodeoxyuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(Br)=C1 WOVKYSAHUYNSMH-RRKCRQDMSA-N 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- NMJREATYWWNIKX-UHFFFAOYSA-N GnRH Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CC(C)C)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 NMJREATYWWNIKX-UHFFFAOYSA-N 0.000 description 3
- 241000700159 Rattus Species 0.000 description 3
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 3
- 230000003042 antagnostic effect Effects 0.000 description 3
- 239000003246 corticosteroid Substances 0.000 description 3
- 229960001334 corticosteroids Drugs 0.000 description 3
- 108091008039 hormone receptors Proteins 0.000 description 3
- 230000002757 inflammatory effect Effects 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 230000029849 luteinization Effects 0.000 description 3
- 108020004999 messenger RNA Proteins 0.000 description 3
- 210000000056 organ Anatomy 0.000 description 3
- 230000001575 pathological effect Effects 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- 239000000523 sample Substances 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 102100032187 Androgen receptor Human genes 0.000 description 2
- WOVKYSAHUYNSMH-UHFFFAOYSA-N BROMODEOXYURIDINE Natural products C1C(O)C(CO)OC1N1C(=O)NC(=O)C(Br)=C1 WOVKYSAHUYNSMH-UHFFFAOYSA-N 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 108010007005 Estrogen Receptor alpha Proteins 0.000 description 2
- 108010041356 Estrogen Receptor beta Proteins 0.000 description 2
- 102100029951 Estrogen receptor beta Human genes 0.000 description 2
- 206010016717 Fistula Diseases 0.000 description 2
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 2
- 102100033417 Glucocorticoid receptor Human genes 0.000 description 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- 206010067572 Oestrogenic effect Diseases 0.000 description 2
- 206010054827 Peritoneal lesion Diseases 0.000 description 2
- 238000010240 RT-PCR analysis Methods 0.000 description 2
- 241000283984 Rodentia Species 0.000 description 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 2
- 230000003187 abdominal effect Effects 0.000 description 2
- 239000003470 adrenal cortex hormone Substances 0.000 description 2
- 230000001270 agonistic effect Effects 0.000 description 2
- 108010080146 androgen receptors Proteins 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 230000001833 anti-estrogenic effect Effects 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 238000001574 biopsy Methods 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 229950004398 broxuridine Drugs 0.000 description 2
- 239000002299 complementary DNA Substances 0.000 description 2
- AZFLJNIPTRTECV-FUMNGEBKSA-N dienogest Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@](CC3)(O)CC#N)CC3)C3=C21 AZFLJNIPTRTECV-FUMNGEBKSA-N 0.000 description 2
- 229960003309 dienogest Drugs 0.000 description 2
- 230000001882 diuretic effect Effects 0.000 description 2
- -1 eplerenone oxime Chemical class 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- 230000003890 fistula Effects 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 239000003018 immunosuppressive agent Substances 0.000 description 2
- 229940125721 immunosuppressive agent Drugs 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 230000003903 intestinal lesions Effects 0.000 description 2
- 150000002576 ketones Chemical class 0.000 description 2
- 229960004400 levonorgestrel Drugs 0.000 description 2
- 229920005610 lignin Polymers 0.000 description 2
- 238000011866 long-term treatment Methods 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 description 2
- 210000004379 membrane Anatomy 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 230000002611 ovarian Effects 0.000 description 2
- QNGNSVIICDLXHT-UHFFFAOYSA-N para-ethylbenzaldehyde Natural products CCC1=CC=C(C=O)C=C1 QNGNSVIICDLXHT-UHFFFAOYSA-N 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 238000011809 primate model Methods 0.000 description 2
- 230000001072 progestational effect Effects 0.000 description 2
- 238000010839 reverse transcription Methods 0.000 description 2
- 241000894007 species Species 0.000 description 2
- 238000011285 therapeutic regimen Methods 0.000 description 2
- 235000021419 vinegar Nutrition 0.000 description 2
- 239000000052 vinegar Substances 0.000 description 2
- ORKBYCQJWQBPFG-WOMZHKBXSA-N (8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 ORKBYCQJWQBPFG-WOMZHKBXSA-N 0.000 description 1
- MXBCYQUALCBQIJ-RYVPXURESA-N (8s,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-11-methylidene-1,2,3,6,7,8,9,10,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-ol;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 MXBCYQUALCBQIJ-RYVPXURESA-N 0.000 description 1
- MXHRCPNRJAMMIM-SHYZEUOFSA-N 2'-deoxyuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 MXHRCPNRJAMMIM-SHYZEUOFSA-N 0.000 description 1
- 208000004998 Abdominal Pain Diseases 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 102000015427 Angiotensins Human genes 0.000 description 1
- 108010064733 Angiotensins Proteins 0.000 description 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 1
- 101100298225 Caenorhabditis elegans pot-2 gene Proteins 0.000 description 1
- 108010072220 Cyclophilin A Proteins 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 208000005171 Dysmenorrhea Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 206010058314 Dysplasia Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 108010020437 Ki-67 Antigen Proteins 0.000 description 1
- 108010000817 Leuprolide Proteins 0.000 description 1
- 206010027304 Menopausal symptoms Diseases 0.000 description 1
- 208000019255 Menstrual disease Diseases 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 206010028594 Myocardial fibrosis Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 208000004880 Polyuria Diseases 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 102100034836 Proliferation marker protein Ki-67 Human genes 0.000 description 1
- 102100028255 Renin Human genes 0.000 description 1
- 108090000783 Renin Proteins 0.000 description 1
- 208000017442 Retinal disease Diseases 0.000 description 1
- 206010038923 Retinopathy Diseases 0.000 description 1
- 208000028347 Sinus disease Diseases 0.000 description 1
- MUCRYNWJQNHDJH-OADIDDRXSA-N Ursonic acid Chemical compound C1CC(=O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CC[C@@H](C)[C@H](C)[C@H]5C4=CC[C@@H]3[C@]21C MUCRYNWJQNHDJH-OADIDDRXSA-N 0.000 description 1
- 206010052428 Wound Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- AUYLVPGDOVEOML-UHFFFAOYSA-N [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(piperidin-1-ylmethoxy)phenyl]methanone Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 AUYLVPGDOVEOML-UHFFFAOYSA-N 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 229940046836 anti-estrogen Drugs 0.000 description 1
- 239000003420 antiserotonin agent Substances 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 229960000817 bazedoxifene Drugs 0.000 description 1
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 description 1
- 230000033558 biomineral tissue development Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 229960003950 combination of corticosteroids Drugs 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 description 1
- 229960000978 cyproterone acetate Drugs 0.000 description 1
- RPLCPCMSCLEKRS-BPIQYHPVSA-N desogestrel Chemical compound C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 RPLCPCMSCLEKRS-BPIQYHPVSA-N 0.000 description 1
- 229960004976 desogestrel Drugs 0.000 description 1
- MXHRCPNRJAMMIM-UHFFFAOYSA-N desoxyuridine Natural products C1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 MXHRCPNRJAMMIM-UHFFFAOYSA-N 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 150000001993 dienes Chemical class 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 239000012636 effector Substances 0.000 description 1
- 239000000328 estrogen antagonist Substances 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 230000035558 fertility Effects 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 229940065346 hydroxyprogesterone acetate Drugs 0.000 description 1
- 230000002267 hypothalamic effect Effects 0.000 description 1
- 238000009802 hysterectomy Methods 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 238000011532 immunohistochemical staining Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 150000002596 lactones Chemical class 0.000 description 1
- 238000002357 laparoscopic surgery Methods 0.000 description 1
- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 description 1
- 229960004338 leuprorelin Drugs 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 239000003550 marker Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000008774 maternal effect Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000002175 menstrual effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- VKHAHZOOUSRJNA-GCNJZUOMSA-N mifepristone Chemical compound C1([C@@H]2C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]3CC[C@@]([C@]3(C2)C)(O)C#CC)=CC=C(N(C)C)C=C1 VKHAHZOOUSRJNA-GCNJZUOMSA-N 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 230000011278 mitosis Effects 0.000 description 1
- 230000000394 mitotic effect Effects 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 238000009806 oophorectomy Methods 0.000 description 1
- 229940127234 oral contraceptive Drugs 0.000 description 1
- 239000003539 oral contraceptive agent Substances 0.000 description 1
- 230000011599 ovarian follicle development Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 210000003101 oviduct Anatomy 0.000 description 1
- 229960005489 paracetamol Drugs 0.000 description 1
- 239000004031 partial agonist Substances 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 230000001991 pathophysiological effect Effects 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 210000004303 peritoneum Anatomy 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 230000001817 pituitary effect Effects 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- RJKFOVLPORLFTN-UHFFFAOYSA-N progesterone acetate Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 RJKFOVLPORLFTN-UHFFFAOYSA-N 0.000 description 1
- 239000000044 progesterone antagonist Substances 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000011552 rat model Methods 0.000 description 1
- 229940075993 receptor modulator Drugs 0.000 description 1
- 230000009711 regulatory function Effects 0.000 description 1
- 230000008085 renal dysfunction Effects 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 238000002271 resection Methods 0.000 description 1
- 238000011808 rodent model Methods 0.000 description 1
- 239000004576 sand Substances 0.000 description 1
- 210000002955 secretory cell Anatomy 0.000 description 1
- 239000000900 selective estrogen receptor beta agonist Substances 0.000 description 1
- 229940121356 serotonin receptor antagonist Drugs 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 230000035946 sexual desire Effects 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- 239000013585 weight reducing agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102007011105A DE102007011105A1 (de) | 2007-03-02 | 2007-03-02 | Mineralcorticoid-Rezeptor-Antagonisten zur Behandlung von Endometriose |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW200900080A true TW200900080A (en) | 2009-01-01 |
Family
ID=39431148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW097107235A TW200900080A (en) | 2007-03-02 | 2008-02-29 | Mineralcorticoid receptor antagonists for the treatment of endometriosis |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20110003778A1 (fr) |
| EP (1) | EP2131825A1 (fr) |
| JP (1) | JP2010520178A (fr) |
| KR (1) | KR20090119870A (fr) |
| CN (1) | CN101621995A (fr) |
| AR (1) | AR065585A1 (fr) |
| AU (1) | AU2008223859A1 (fr) |
| BR (1) | BRPI0808427A2 (fr) |
| CA (1) | CA2679520A1 (fr) |
| DE (1) | DE102007011105A1 (fr) |
| IL (1) | IL200380A0 (fr) |
| MX (1) | MX2009009332A (fr) |
| RU (1) | RU2009136305A (fr) |
| TW (1) | TW200900080A (fr) |
| WO (1) | WO2008107373A1 (fr) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI1003661A2 (pt) * | 2010-09-15 | 2013-01-08 | Libbs Farmaceutica Ltda | associaÇço farmacÊutica para tratar e/ou prevenir mioma e/ou endometriose, uso de resveratrol e progestogenio, composiÇço farmacÊutica para tratamento e/ou prevenÇço de mioma e/ou endometriose medicamento para tratamento e/ou prevenÇço de mioma e/ou endometrios, kit e mÉtodo para tratamento e/ou prevenÇço de mioma e/ou endometriose |
| CA2854215A1 (fr) | 2011-11-04 | 2013-05-10 | Bayer Pharma Aktiengesellschaft | 18-methyl-6,7-methylene-3-oxo-17-pregn-4-ene-21,17?-carbolactones, preparations pharmaceutiques contenant ces composes et leur utilisation dans le traitement de l'endometriose |
| TW201350122A (zh) * | 2012-04-23 | 2013-12-16 | Bayer Pharma AG | １８－甲基－１５β，１６β－亞甲基－１９－降－２０－螺氧－４－烯－３－酮的子宮內用途，包含１８－甲基－１５β，１６β－亞甲基－１９－降－２０－螺氧－４－烯－３－酮的子宮內系統，及其於避孕及婦科治療之用途 |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| WO2014115449A1 (fr) * | 2013-01-22 | 2014-07-31 | シャープ株式会社 | Dispositif d'affichage à cristaux liquides |
| TW201607943A (zh) | 2013-12-19 | 2016-03-01 | 拜耳製藥公司 | 作為ｅｐ４配體之新穎苯并咪唑衍生物 |
| CN117959293B (zh) * | 2024-01-18 | 2025-05-13 | 香港大学深圳医院 | 非奈利酮在制备治疗和/或预防卵巢功能障碍疾病药物中的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4042004A1 (de) * | 1990-12-22 | 1992-06-25 | Schering Ag | 14(beta)-h-, 14- u. 15-en-11(beta)-aryl-4-estrene |
| DE4042005A1 (de) * | 1990-12-22 | 1992-06-25 | Schering Ag | D-homo-(16-en)-11(beta)-aryl-4-estrene |
| DK1229906T3 (da) | 1999-08-31 | 2008-02-11 | Bayer Schering Pharma Ag | Mesoprogestiner til behandlingen og forebyggelsen af godartede, hormonafhængige, gynækologiske lidelser |
| KR100913910B1 (ko) | 2000-01-18 | 2009-08-26 | 바이엘 쉐링 파마 악티엔게젤샤프트 | 호르몬 보충 요법용 드로스피렌온 |
| EP1535618A1 (fr) * | 2003-11-26 | 2005-06-01 | Schering Aktiengesellschaft | Préparation pharmaceutique pour le traitement hormonal continuel sur plus de 21-28 jours comprenant deux compositions d'estrogène et/ou de progestine |
| MY151322A (en) * | 2004-04-30 | 2014-05-15 | Bayer Ip Gmbh | Management of breakthrough bleeding in extended hormonal contraceptive regimens |
| FR2886151B1 (fr) * | 2005-05-31 | 2007-09-07 | Mayoly Spindler Soc Par Action | Utilisation de la colchicine pour la preparation d'un medicament destine a la prevention et/ou au traitement de l'endometriose |
-
2007
- 2007-03-02 DE DE102007011105A patent/DE102007011105A1/de not_active Withdrawn
-
2008
- 2008-02-28 US US12/529,447 patent/US20110003778A1/en not_active Abandoned
- 2008-02-28 KR KR1020097018145A patent/KR20090119870A/ko not_active Ceased
- 2008-02-28 MX MX2009009332A patent/MX2009009332A/es active IP Right Grant
- 2008-02-28 RU RU2009136305/15A patent/RU2009136305A/ru not_active Application Discontinuation
- 2008-02-28 EP EP08717238A patent/EP2131825A1/fr not_active Withdrawn
- 2008-02-28 AU AU2008223859A patent/AU2008223859A1/en not_active Abandoned
- 2008-02-28 CN CN200880006913A patent/CN101621995A/zh active Pending
- 2008-02-28 CA CA002679520A patent/CA2679520A1/fr not_active Abandoned
- 2008-02-28 WO PCT/EP2008/052456 patent/WO2008107373A1/fr not_active Ceased
- 2008-02-28 BR BRPI0808427-0A patent/BRPI0808427A2/pt not_active IP Right Cessation
- 2008-02-28 JP JP2009551220A patent/JP2010520178A/ja active Pending
- 2008-02-29 TW TW097107235A patent/TW200900080A/zh unknown
- 2008-03-03 AR ARP080100887A patent/AR065585A1/es unknown
-
2009
- 2009-08-13 IL IL200380A patent/IL200380A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2009136305A (ru) | 2011-04-10 |
| BRPI0808427A2 (pt) | 2014-07-22 |
| AU2008223859A1 (en) | 2008-09-12 |
| EP2131825A1 (fr) | 2009-12-16 |
| IL200380A0 (en) | 2010-04-29 |
| US20110003778A1 (en) | 2011-01-06 |
| WO2008107373A1 (fr) | 2008-09-12 |
| AR065585A1 (es) | 2009-06-17 |
| JP2010520178A (ja) | 2010-06-10 |
| CA2679520A1 (fr) | 2008-09-12 |
| MX2009009332A (es) | 2009-09-11 |
| KR20090119870A (ko) | 2009-11-20 |
| DE102007011105A1 (de) | 2008-09-04 |
| CN101621995A (zh) | 2010-01-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Sitruk-Ware et al. | The use of newer progestins for contraception | |
| Sitruk-Ware | New progestogens: a review of their effects in perimenopausal and postmenopausal women | |
| Schürmann et al. | Estradiol and drospirenone for climacteric symptoms in postmenopausal women: a double-blind, randomized, placebo-controlled study of the safety and efficacy of three dose regimens | |
| US10201611B2 (en) | Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy | |
| TW200900080A (en) | Mineralcorticoid receptor antagonists for the treatment of endometriosis | |
| TW201322986A (zh) | １８－甲基－６，７－亞甲基－３－氧基－１７－妊－４－烯－２１，１７β－羧內酯、包含該化合物之醫療製劑及其於治療子宮內膜異位症之用途 | |
| ME01123B (me) | Režim doziranja antiprogestina | |
| ME01122B (me) | Jedinjenja i postupci za liječenje raka dojke | |
| Cleve et al. | Pharmacology and clinical use of sex steroid hormone receptor modulators | |
| KR20090067198A (ko) | 자궁내막 증식을 억제하는 조성물과 방법 | |
| Sabbadin et al. | Spironolactone and intermenstrual bleeding in polycystic ovary syndrome with normal BMI | |
| US20040087563A1 (en) | Hormone replacement therapy with cardiovascular protection using antialdosteronic progestins | |
| Shields-Botella et al. | An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells | |
| KR100864547B1 (ko) | 양성 호르몬 의존성 부인과 질병의 치료 및 예방을 위한메조프로게스틴 (프로게스테론 수용체 조절물질) | |
| Sitruk-Ware et al. | Role of progestins with partial antiandrogenic effects | |
| EP0654267B1 (fr) | Agent carcinostatique pour thérapie harmonale contenant du dienogest comme composant actif | |
| HK1139602A (en) | Mineralcorticoid receptor antagonists for the treatment of endometriosis | |
| TW200927137A (en) | Compositions and methods for treating dysfunctional uterine bleeding | |
| JP2005521665A (ja) | 心血管障害の予防および治療のための、アルドステロンアンタゴニストおよび非ステロイド系抗炎症剤の併用治療 | |
| WO2004041288A1 (fr) | Therapie de remplacement d'hormone a l'aide de drospirenone | |
| TW200950788A (en) | Compositions and methods for male contraception | |
| Millán et al. | Sex Hormones and Related Compounds, Including Hormonal Contraceptives | |
| BE1027858A1 (fr) | Composition pharmaceutique pour la contraception chez la femme | |
| Archer | Aging of the endometrium | |
| Kurabayashi et al. | P061 Association of the ß3-adrenergic receptor gene TRP64ARG mutation with weight, body mass index, abdominal fat, blood pressure and reproduction |